PROCATEROL HYDROCHLORIDE Chemical Properties

storage temp. 

2-8°C

solubility 

Soluble to 100 mM in water and to 100 mM in DMSO

form 

Powder

color 

White to off-white

Stability:

Hygroscopic

InChI

1S/C16H22N2O3.ClH/c1-4-12(17-9(2)3)16(21)11-5-7-13(19)15-10(11)6-8-14(20)18-15;/h5-9,12,16-17,19,21H,4H2,1-3H3,(H,18,20);1H/t12-,16+;/m0./s1

InChIKey

AEQDBKHAAWUCMT-CVHDTDHSSA-N

SMILES

Cl.CC[C@H](NC(C)C)[C@H](O)c1ccc(O)c2NC(=O)C=Cc12

Safety Information

WGK Germany 

2

RTECS 

VC8296000

Storage Class

11 - Combustible Solids

PROCATEROL HYDROCHLORIDE Usage And Synthesis

Description

Procaterol is an agonist of β₂-adrenergic receptors (β₂-ARs). It binds to (K_d = 46 pM), and is selective for, β₂-ARs over β₁-ARs (K_d = 4,000 pM). Procaterol binds more potently to β₂-ARs in isolated guinea pig lung than to β₁-ARs in isolated guinea pig cardiac ventricle in the presence (IC_50s = 175 and 1,660 nM, respectively) and absence of GTP (; IC₅₀s = 55.1 and 1,660 nM, respectively). It inhibits contractions induced by acetylcholine in isolated guinea pig trachea (EC₅₀ = 10.5 nM). In vivo, procaterol inhibits histamine-induced airflow obstruction in a guinea pig model of ovalbumin-sensitized asthma when administered via inhalation at a dose of 10 μg/ml.

Uses

adrenergic agonists

Uses

Procaterol Hydrochloride is a short-acting pulmonary β2-agonist for asthma treatment.

General Description

Procaterol is used to prevent lung fibroblast migration. It has anti-inflammatory properties. It can block type 2 T helper (Th2)-related chemokine production in human monocytes and bronchial epithelial cells.

Biological Activity

Specific and very potent β 2 agonist.

Biochem/physiol Actions

β2-adrenoceptor agonist; bronchodilator.

storage

Store at RT

References

[1] S MARULLO. Selective binding of ligands to beta 1, beta 2 or chimeric beta 1/beta 2-adrenergic receptors involves multiple subsites.[J]. EMBO Journal, 1990, 9 5: 1471-1476. DOI: 10.1002/j.1460-2075.1990.tb08264.x
[2] HIDEO KIKKAWA  Katsuo I  Kazuaki Naito. Tracheal Relaxing Effects and β2-Selectivity of TA-2005, a Newly Developed Bronchodilating Agent, in Isolated Guinea Pig Tissues[J]. Japanese journal of pharmacology, 1991, 57 2: Pages 175-185. DOI: 10.1254/jjp.57.175
[3] SHIRO YOSHIZAKI. Sympathomimetic amines having a carbostyril nucleus[J]. Journal of Medicinal Chemistry, 1976, 19 9: 1138-1142. DOI: 10.1021/jm00231a011
[4] MIRZA. Inhaled procaterol inhibits histamine-induced airflow obstruction and microvascular leakage in guinea-pig airways with allergic inflammation[J]. Clinical and Experimental Allergy, 2008, 28 5: 644-652. DOI: 10.1046/j.1365-2222.1998.00263.x

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